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UVRAG is a mammalian ortholog of
2019-10-21

UVRAG is a mammalian ortholog of yeast Vps38 and a promoter of autophagy [51,60,61]. It forms distinct complexes with BECN1 (mammalian ortholog of yeast Vps30/Atg6) and the class III phosphatidylinositol 3-kinase (whose catalytic subunit [PIK3C3] is the mammalian ortholog of yeast Vps34) and contrib
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In our former work our interest was in
2019-10-21

In our former work, our interest was in discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Along this line, with natural alkaloid taspine as the lead compound, rounds of structure optimization were performed to develop novel VEGFR-2 inhibitors [[13], [14], [15]]. Among them, BPS-7,
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br Experimental procedures br Results Fluorescence attributa
2019-10-21

Experimental procedures Results Fluorescence attributable to GnRH-eGFP neurons was observed through the diagonal band of Broca, to the POA of the hypothalamus in GnRH-eGFP transgenic rats for all groups as described previously (Kato et al., 2003, Tada et al., 2013). Discussion The mEPSCs w
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Enolases are among the most abundantly expressed cytosolic
2019-10-21

Enolases are among the most abundantly expressed cytosolic proteins. They are metalloenzymes that catalyze the conversion of 2-phosphoglycerate to phosphoenolpyruvate [18]. Eubacteria and archaebacteria have a single enolase gene (reviewed in [19]). Despite the lack of signal peptides or cognate pro
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In general cellular senescence is
2019-10-21

In general, cellular senescence is considered a programmed response to stress that can be activated by oxidative stress, irradiation or action of substances or drugs. These stressors cause DNA damage and, through the action of specific proteins (p53 and p21), lead to cell senescence (di Fagagna, 200
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The UPP broadly involves proteolysis
2019-10-21

The UPP broadly involves proteolysis in biochemical processes and is a potential target for cancer therapy. The UPP degrades unfolding or damaged proteins by an ATP-dependent mechanism (Ciechanover, Elias, Heller, Ferber, & Hershko, 1980). It also plays an important role in Histamine Phosphate mg re
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A different example of substrate dependent activation is
2019-10-21

A different example of substrate-dependent activation is seen in CSN5, a JAMM-type DUB found in the eight subunit COP9 signalosome (CSN) [34]. The CSN deconjugates NEDD8 (neural precursor cell expressed developmentally downregulated 8) from Cullin Ring ubiquitin E3 ligases (CRLs). Through this activ
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topotecan Sensory gating describes a filter mechanism protec
2019-10-19

‘Sensory gating’ describes a filter mechanism protecting the central nervous system from sensory overload by inhibiting behaviorally irrelevant input (Boutros et al., 2004, 2008). This permits topotecan to a changing contextual environment (Fruhstorfer et al., 1970; Grunwald et al., 2003). Auditory
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The nucleus accumbens is a critical locus
2019-10-19

The nucleus accumbens is a critical locus for ER/mGluR signaling in the context of addiction ER/mGluR signaling is regulated by caveolin proteins and palmitoylation Because of the vast implications of ER/mGluR association, it is important to understand what regulates their interaction. Such regu
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Other studies have investigated the role
2019-10-19

Other studies have investigated the role of HDAC inhibitors in particular signaling pathways mediated by EWS–FLI1 (Matsumoto et al., 2001). A recent investigation, showed a physical association of EWS–FLI1 and HDAC1 that helps mediate a disruption in the p53 activation of downstream targets (Li et
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The biological actions of ET are
2019-10-19

The biological actions of ET‐1 are mediated via two distinct receptor subtypes, the endothelin A and endothelin B receptors (ETA/ETB). While activation of ETA is assumed to mediate contraction of smooth muscle cells, the activity of ETB is related to transient vasodilation [22]. In human corpus cave
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In conclusion our findings demonstrated that S PC
2019-10-19

In conclusion, our findings demonstrated that S1PC augments HMOX1 expression in a NO-dependent manner, and its effects are associated with the enhancement of BACH1 degradation. In addition, S1PC and NO potentially degrade BACH1 based on the observation that nuclear degradation of BACH1 differs from
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Herein the interactions of etamicastat nepicastat and zamica
2019-10-18

Herein, the interactions of etamicastat, nepicastat and zamicastat with P-gp and BCRP were evaluated. Although recent investigations have been performed to assess the involvement of P-gp in the BHQ exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of BCRP remains unde
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There was a good alignment profile between
2019-10-18

There was a good alignment profile between compound 26 (IC50 0.06μM) and MTX (IC50 0.08μM) explaining its activity pattern (Fig. 5a). Fig. 5b clearly indicates a different alignment profiles where carbonyl groups are not on the same side between 25 (IC50>100.0μM) and MTX which is in consistency with
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First we synthesized inhibitor following the patent
2019-10-18

First, we synthesized inhibitor following the patent procedure reported by Shewchuk et al. to provide its first complete characterization (see ). Two different synthetic approaches were used to obtain compounds –. The first method relied on the alkylation of the common 5-phenol-2,4-diaminopyrimidin
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